穆坪马兜铃化学成分的研究

自穆坪马兜铃(Aristolochia moupinensis Franch)根、茎中分得十三个化合物,其中化合物Ⅰ～Ⅻ经鉴定分別为马兜铃酸Ⅰ(aristolochic acid Ⅰ)(Ⅰ),尿囊素(allantoin)(Ⅱ),紫丁香酸(syringic acid)(Ⅲ),香豆酸(P-coumaric acid)(Ⅳ),马兜铃酸Ⅳ(aristolochic acid Ⅳ)(Ⅴ),β-谷甾醇(Ⅵ),木兰碱(magnoflorine)(Ⅶ),马兜铃酸Ⅳ甲醚aristolochic acid Ⅳmethyl ether(Ⅵ),棕榈酸(Ⅸ),马兜铃酸Ⅱ(aristolochic acid Ⅱ)(Ⅹ),N(Phydroxyphenethy1)P-coumaramide(Ⅺ),马兜铃酸Ⅳ甲醚甲酯(aristolochic acid Ⅳmethyl ether methyl ester)(Ⅻ),化合物ⅩⅢ为新化合物,经光谱分析和化学合成等方法证明其结构为N(P-hydroxyphenethyl)-ferulamide,命名为穆坪马兜铃酰胺(moupinamide)。初步药理试验表明穆坪马兜铃酰胺体外有抑制血小板聚集和影响血小板内前列腺素合成的作用。     

管花马兜铃化学成分的研究

从管花马兜铃(Aristolchia tubflora Dunn)中分得一个新化合物,经光谱(IR,UV,HRMS,HNMR,NOEDS)鉴定为9,1O-二羟基-8-甲氧基-3,4-亚甲二氧基菲-1-羧酸-内酯,命名为马兜铃菲内酯I;另七个马兜铃菲类化合物是马兜铃酸Ⅰ,Ⅱ,Ⅲa,Ⅶa,马兜铃内酰胺Ⅰ,Ⅱ及青木香酸。     

马兜铃酸的倍半萜的酯类化合物VI.绵毛马兜铃中马兜铃酸萜酯I的结构鉴定

从绵毛马兜铃(Aristolocha mannisima Hance)中分得一个马兜铃酸倍半萜的酯类化合物,经红外、紫外、高分辩质谱和多种一维和二维核磁共振谱鉴定,确定了其骨架结构及顺反构型,命名为马兜铃酸萜酯I。     

大环骨架结构的倍半萜化合物——Ⅵ.马兜铃新内酯的化学结构测定

自绵毛马兜铃(Aristolochia mollissima Hance)根茎中分得九个化合物,其中已报道的七个化合物是尿囊素、马兜铃内酯、绵毛马兜铃内酯、β-谷甾醇、马兜铃酸A、9-乙氧基马兜铃内酯和9-乙氧基马兜铃内酰胺,本文报道结晶K₃的化学结构,经光谱分析(IR,¹H-NMR,¹³C-NMR,2D-NMR和MS),化学反应及X-衍射晶体分析,确证K₃为一个新骨架结构的倍半萜化合物,命名为马兜铃新内酯。     

穆坪马兜铃化学成分的研究

自穆坪马兜铃(Aristolochia moupinensis Franch)根、茎中分得十三个化合物,其中化合物Ⅰ～Ⅻ经鉴定分別为马兜铃酸Ⅰ(aristolochic acid Ⅰ)(Ⅰ),尿囊素(allantoin)(Ⅱ),紫丁香酸(syringic acid)(Ⅲ),香豆酸(P-coumaric acid)(Ⅳ),马兜铃酸Ⅳ(aristolochic acid Ⅳ)(Ⅴ),β-谷甾醇(Ⅵ),木兰碱(magnoflorine)(Ⅶ),马兜铃酸Ⅳ甲醚aristolochic acid Ⅳ methyl ether(Ⅵ),棕榈酸(Ⅸ),马兜铃酸Ⅱ(aristolochic acid Ⅱ)(Ⅹ),N(Phydroxyphenethy1)P-coumaramide(Ⅺ),马兜铃酸Ⅳ甲醚甲酯(aristolochic acid Ⅳ methyl ether methyl ester)(Ⅻ),化合物ⅩⅢ为新化合物,经光谱分析和化学合成等方法证明其结构为N(P-hydroxyphenethyl)-ferulamide,命名为穆坪马兜铃酰胺(moupinamide)。 初步药理试验表明穆坪马兜铃酰胺体外有抑制血小板聚集和影响血小板内前列腺素合成的作用。     

绵毛马兜铃化学成分研究——Ⅳ.绵毛马兜铃内酯的化学结构测定

从马兜铃属植物绵毛马兜铃Aristolochia mollissima Hance根茎中分得9种(Ⅰ～Ⅸ)成分,其中结晶Ⅲ为一新倍半萜内酯,用光谱法测定了化学结构,命名为绵毛马兜铃内酯Mollislactone,晶Ⅰ为尿囊素,晶Ⅱ为马兜铃内酯,晶Ⅳ为β-谷甾醇,晶Ⅸ为马兜铃酸,其余成分尚在研究中。     

黄花远志根化学成分的分离和结构鉴定

从黄花远志(Polygala arilata Buch-Ham.)根中分离得到7个化合物,根据光谱(UV,IR,MS,¹HNMR,DIFNOE和¹³CNMR)解析和理化性质,分别鉴定为1-甲氧基-2,3-亚甲二氧基口山酮(I)、1,7-二羟基-2,3-亚甲二氧基口山酮(II)、1,6,7-三羟基-2,3-二甲氧基口山酮(II)、对羟基苯甲酸(IV)、远志醇(V)、豆甾醇(VI)、豆甾醇β-D-吡喃葡萄糖甙(VII)。其中,I和II为新化合物,VI和VI为首次从该植物中分得。化合物I～II有抑制醛糖酶的作用。     

5α-△9(11)-16β-甲基-3β,17α,21-三羟基-孕甾烯-3β,21-双醋酸酯-20酮和5α,17α-甲基-17β-羟基-雄甾-3酮的微生物转化

用诺卡氏菌与节杆菌混合菌种转化从蕃麻皂素制得的中间体5α-△⁹⁽¹¹⁾-16-16β-甲基-3β,17α,21三羟基孕甾烯-3β,21-双醋酸酯-20酮(Ⅰ)得50%的16β-甲基-△^1,4,9(11)-孕甾三烯-20酮(Ⅱ)和少量的16β-甲基-9,11α环氧-△¹,4孕甾二烯-20酮(Ⅲ)。另外,又用同样的混合菌种转化从剑麻皂素制得的中间体5α,17α甲基-17β羟基-雄甾-3酮(Ⅳ)得50%17α甲基-17β羟基-△^1,4-雄甾二烯-3酮(Ⅴ)。如改变培养基则得3,17β-羟基-17α-甲基-9酮基-9,10开环-1,3,5(10)雄甾三烯化合物。     

毛叶假鹰爪根化学成分的研究

目的：寻找番荔枝科假鹰爪属植物毛叶假鹰爪［Desmos dumosus (Roxb.) Saff］根抗肿瘤活性成分。方法：用硅胶柱色谱分离化学成分;UV,IR,EI-MS,¹HNMR,¹³CNMR,¹H-¹H COSY,HMQC,HMBC,NOESY等方法鉴定结构。结果：从氯仿萃取物中分离鉴定了6个化合物,分别为2-甲氧基-3-甲基-4,6-二羟基-5-(3′-羟基)肉桂酰基苯甲醛(I),5-羟基-7-甲氧基-8-甲酰基-3-苯甲酰基-2,6-二甲基-2S,3R-二氢色原酮(II),豆甾-4-烯-3,6-二酮(III),豆甾烷-3,6-二酮(IV),荠宁黄酮(V),黄芩素-7-甲醚(VI)。结论：化合物II为新化合物,命名为毛叶假鹰爪素A。I,III和IV为首次从本种植物中得到。III有细胞毒活性。     

5α-△9(11)-16α-甲基-3β,17α,21-三羟基-孕甾烯-3β,21-双醋酸酯-20酮的微生物转化

简单节杆菌A₁及耻垢杆菌MS₁两种菌混合培养转化地塞米松中间体5α-△⁹⁽¹¹⁾-16α-甲基-3μ,17μ,21-三羟基-孕甾烯-3μ,21-双醋酸酯-20酮(Ⅲ)可得到16α-甲基-△^1.4.0(11)-孕甾烯-17α,21-双羟基-3,20双酮(Ⅳ)(65%收率)及少量的16α-甲基-△^1.4孕甾烯-9α,11α-环氧-17α,21双羟基-3,20双酮(Ⅴ)。     

滇藏荨麻根中化学成分的分离与鉴定

目的研究荨麻属植物滇藏荨麻的化学成分。方法运用硅胶柱色谱、薄层色谱、制备薄层色谱S、ephadex LH-20柱色谱等方法进行分离纯化,通过理化性质和1H-NMR1、3C-NMR、EI-MS等数据以及与对照品对照等方法进行结构鉴定。结果从滇藏荨麻根分离得到10个化合物,分别鉴定为:豆甾-4-烯-3-酮(1)、4-羟基反式桂皮酸(2)、4-羟基苯甲醛(3)、4-甲氧基苯甲酸(4)、4-羟基苯甲酸(5)、己二酸(6)、二十四烷酸甲酯(7)、2-羟基二十四烷酸甲酯(8)、胡萝卜苷(9)、β-谷甾醇(10)。结论化合物1~10均为首次从滇藏荨麻中分离得到,其中化合物4、6~8为首次从荨麻属植物中分离得到。     

马兜铃属植物的化学(Ⅱ)异马兜铃酸与马兜铃酸的关系

作者等前于土青木香(Aristolochia debilis, S. et Z.)中分出一种m.p. 275℃(分解)的黄色结晶(Ⅰ),从其元素分析、游离酸及其甲酯的熔点看来,均与異马兜铃酸(Ⅱ)一致.经继续研究,证明(Ⅰ)应与马兜铃酸(Ⅲ)相同,因此作这二种化合物的检查.按马兜铃酸是马兜铃属植物的一个共有成分,而異马兜铃酸则系1935年Krishnaswamy,Manjunath,Rao等氏从印度马兜铃(A. indica)中分出.Rosenmund,Reichstein等曾怀疑这二种成分可能是同一化合物,但没有充分的证据。     

群海绵Agelas sp.的化学成分研究

目的 研究海绵Agelas sp.的化学成分。方法 运用乙醇提取、硅胶、Sephadex-LH₂₀色谱柱、HPLC等多种方法进行分离和纯化,根据理化性质和波谱数据进行结构鉴定。结果 分离得到9个化合物,经结构鉴定分别为4,5-二溴吡咯-2-甲酰胺（1）、4,5-二溴吡咯-2-甲酸（2）、4,5-二溴吡咯-2-甲酸甲酯（3）、N-（4,5-二溴-2-吡咯甲酰基）甘氨酸甲酯（4）、1-（4,5-二溴-2-吡咯甲酰胺基）丙酸甲酯（5）、1-（4,5-二溴-2-吡咯甲酰胺基）丙酸乙酯（6）、异吲哚-1,3-二酮（7）、2（3H）-苯并噻唑酮（8）和manzacidin C（9）。结论 化合物4~9为首次从该属海绵中分离得到,其中化合物4~6为新天然产物。     

COMPARISON OF RESPONSES TO AMINOGUANIDINE AND Nω-NITRO-L-ARGININE METHYL ESTER IN THE RAT AORTA

1. We have compared the effect of aminoguanidine with that of N^ω-nitro-L-arginine methyl ester on isolated thoracic aortic rings obtained either from endotoxin (lipopolysaccharide, 10 mg/kg, i.v. for 3 h) or vehicle (saline) treated rats. 2. Administration of endotoxin for 3h resulted in a hypo tension and a significant reduction of pressor responses to nor-epinephrine (1 μg/kg, i.v.) in the anaesthetized rat. 3. In intact rings obtained from vehicle treated rats, amino guanidine (0.3 and 1mmol/L) had no significant effect on acetylcholine-induced relaxation (10^-9–10^-5mol/L), whereas N^ω-nitro-L-arginine methyl ester (0.3mmol/L and 1mmol/L) abolished that response, suggesting that aminoguanidine does not inhibit the activity of constitutive nitric oxide synthase. 4. Relaxation induced by L-arginine (10^-6–10^-2mol/L) was competitively inhibited by both aminoguanidine (0.3 mmol/L) and N^ω-nitro-L-arginine methyl ester (0.3 mmol/L) in endo thelium-denuded aortic rings obtained from endotoxin treated rats. 5. Three hours of endotoxaemia was associated with an impairment of contraction to norepinephrine (10^-9–10^-6 mol/L) in the endothelium-denuded aorta ex vivo. This hyporeactivity to norepinephrine was partially restored by treatment of the vessels either with aminoguanidine (0.3 mmol/L) or with N^ω-nitro-l-arginine methyl ester (0.3 mmol/L) in vitro. 6. These results in isolated thoracic aortae of the rat reinforce that aminoguanidine is a selective inhibitor of the inducible nitric oxide synthase, whereas N^ω-nitro-L-arginine methyl ester is a non-selective inhibitor of both the inducible and constitutive nitric oxide synthase.     

肿瘤的化学治療 ⅩⅥ.γ-{对-[双-(2-氯乙基)-氨甲基)-苯基}-丁酸和4-{对-[双-(2-氯乙基)-氨甲基]-苯基}-丁醇的合成

自γ-(对氯甲基-苯基)-丁酸(Ⅵ)开始,经过四步反应合成了γ-{对-[双-(2-氯乙基)-氨甲基]-苯基}-丁酸盐酸盐(Ⅳ),此外还合成了化合物(Ⅳ)的甲酯(Ⅺ)和乙酯(Ⅻ)。后者以氢化锂铝还原,生成4-对(-[双-(2-氯乙基)-氨甲基]-苯基)-丁醇盐酸盐(Ⅴ)。上述化合物对肉瘤180无明显的抑制作用。     

牛蒡根乙酸乙酯部位的化学成分研究

摘 要 目的：研究牛蒡根乙酸乙酯部位的化学成分。方法: 采用柱色谱和制备液相等方法对牛蒡根乙酸乙酯部位化学成分进行分离纯化,运用波谱学方法鉴定化合物结构。结果: 从牛蒡根乙酸乙酯部位共分离得到了7个化合物,分别鉴定为: 邻苯二甲酸二丁酯（1）、咖啡酸甲酯（2）、8- 甲氧羰甲基-对羟基肉桂酸（3）、3-O-咖啡酰奎宁酸甲酯（4）、咖啡酸（5）、3,4-O-双咖啡酰奎宁酸甲酯（6-a）和3,5-O-双咖啡酰奎宁酸甲酯（6-b）、乙二醇（7）。结论:确定其中8- 甲氧羰甲基-对羟基肉桂酸（3）为首次从菊科植物中分离获得;3-O-咖啡酰奎宁酸甲酯（4）、3,4-O-双咖啡酰奎宁酸甲酯（6-a）和3,5-O-双咖啡酰奎宁酸甲酯（6-b）为首次从牛蒡属植物中分离得到。     

华钩藤中新的氧化吲哚生物碱甙

自中药华钩藤(Uncaria sinensis[Oliv]Havil)叶子的乙醇提取物中分得2个16-位羧基氧化吲哚生物碱和2个它们的葡萄糖酯甙。经化学和光谱方法(UV,IR,FAB-MS,¹H-NMR,¹³C-NMR,CD)分别鉴定了它们结构,并命名为帽柱木菲酸(mitraphyllic acid,Ⅰ),异帽柱木菲酸(isomitraphyllic acid,Ⅱ),帽柱木菲酸[16-1]-β-D-吡喃葡萄糖酯甙(mitraphyllic acid[16-1]-β-D-glucopyranosyl ester,Ⅳ)和异帽柱木菲酸(16-1)-β-D-吡喃葡萄糖酯甙(isomitraphyllic acid[16-1]-β-D-glucopyranosyl ester,Ⅲ)。除化合物Ⅰ外,其余均为首次从天然得到的新化合物。     

Polygosumic acid,a new cadinane sesquiterpene from <Emphasis Type="Italic">Polygonum viscosum</Emphasis>, inhibits the growth of drug-resistant <Emphasis Type="Italic">Escherichia coli</Emphasis> and <Emphasis Type="Italic">Staphylococcus aureus</Emphasis> (MRSA) in vitro

Three new sesquiterpenes, 6-hydroxy-7-(1-methylethyl)-3,3a,6,7,8,8a-hexahydroazulene-1,4-dicarboxylic acid methyl ester (1, named viscozulenic acid methyl ester), 7-(1-methylethyl)-3,3a,6,7,8,8a-hexahydroazulene-1,4-dicarboxylic acid 1-methyl ester (2, named viscoazucinic acid) and 3-oxo-1-epi-sclerosporin (3, named polygosumic acid), have been isolated from the chloroform extract of the aerial parts of Polygonum viscosum by reversed-phase preparative high performance liquid chromatography (HPLC). The structures of these compounds were established conclusively by ultraviolet (UV), mass spectrometry (MS) and a series of 1D and 2D nuclear magnetic resonance (NMR) analyses. The anti-bacterial properties of 1–3 against 12 pathogenic bacterial strains have also been assessed by the rapid and robust microtitre-plate-based serial dilution method incorporating resazurin as an indicator of cell growth. Polygosumic acid was the most active among the sesquiterpenes and inhibited the growth of penicillin-resistant Escherichia coli (minimum inhibitory concentration, MIC=0.05 mg/ml) and methicillin-resistant Staphylococcus aureus (MRSA) (MIC=0.10 mg/ml).     

疟原虫组织期裂殖体杀灭剂4-甲基-5-(对-氟苯氧基)伯氨喹类似物的合成

A series of. analogues of 4-methyl-5-(p-fluorophenoxy)-primaquine have been prepared for evaluating of tissue schizonticidal actiyity of Plasmodium yoelii in mice. 2-Bromo-4-acetamino-5-nitroanisole was reacted with pfluorophenol in the presence of potassium hydroxide to give 2-(p-fluorophenoxy) 4-acetamino-5-nitroanisole, which was subsequently hydrolyzed to yield corresponding amino compound. Cyclization of the amino compound with methyl vinyl ketone afforded 4-methyl-5-(p-fluorophenoxy)-6-methoxy-8-nitroquinoline. This product was reduced by iron and acetic acid to give corresponding 8-aminoquinoline. The latter was condensed with bromoalkylphthalimides to yield 4-methyl-5-(pfluorophenoxy)-6-methony-8- (1-phthalimidoalkyl) aminoquinolines (Ⅳ₁～Ⅳ₇). These compounds were heated with hydrazine hydrate to form 4-methyl-5-(p-fluorophenoxy)-6-methoxy-8-(1-aminoalkyl)aminoquinolines(Ⅳ₈～Ⅳ₁₃), and 4-methyl-5-(p-fluorophenoxy) primaquine (Ⅱ).Compound Ⅱ synthesized was radical curative at 10 mg/kg×1, while the analogues Ⅳ₉ and Ⅳ₁₀ were radical curative at 100 mg/kg×1 against P. yoelii in mice.